PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
27138546-0	2017	An Exposure-Response Modeling Approach to Examine the Relationship Between Potency of CYP3A Inducer and Plasma 4beta-Hydroxycholesterol in Healthy Subjects.	cholest-5-ene-3,4-diol	111-135	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	86-91
27991741-2	2017	We determined 4beta-hydroxycholesterol (4betaOHC), an endogenous CYP3A4 metabolite, in patients with rheumatoid arthritis (RA) before and after treatment with biological disease-modifying antirheumatic drugs (bDMARDs).	cholest-5-ene-3,4-diol	14-38	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	65-71
27565568-0	2016	Rapid LC-MS/MS method for the determination of 4-hydroxycholesterol/cholesterol ratio in serum as endogenous biomarker for CYP3A activity in human and foals.	cholest-5-ene-3,4-diol	47-67	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	123-128
27777246-6	2017	The sensitive CYP3A biomarker 4beta-hydroxycholesterol is built into the early clinical phase I studies for all candidates since rare cases of in vivo induction have been found without any induction alerts from the currently used in vitro methods.	cholest-5-ene-3,4-diol	30-54	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	14-19
27565568-2	2016	Thus, it was the aim of this study to develop and validate an analytical method allowing estimation of the hepatic CYP3A enzyme activity using the 4-hydroxycholesterol to cholesterol ratio as an endogenous biomarker in serum.	cholest-5-ene-3,4-diol	147-167	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	115-120
27565568-11	2016	Finally, the validated assay was applied to measure 4-hydroxycholesterol and cholesterol in serum samples of clinical studies in humans and foals that could verify induction of hepatic CYP3A4 (human) and CYP3A89 (foals) after premedication with the known enzyme inducer rifampicin.	cholest-5-ene-3,4-diol	52-72	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	185-191
27416363-4	2016	Ezetimibe treatment altered the expression of genes for cholesterol and fatty acid metabolism and decreased the expression of CYP3A46, which catabolizes cholesterol to 4beta-hydroxycholesterol, strongly in liver.	cholest-5-ene-3,4-diol	168-192	cytochrome P450 family 3 subfamily A member 46	Sus scrofa	126-133
27350147-0	2016	Recommendations on the Development of a Bioanalytical Assay for 4beta-Hydroxycholesterol, an Emerging Endogenous Biomarker of CYP3A Activity.	cholest-5-ene-3,4-diol	64-88	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	126-131
27350147-1	2016	The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity.	cholest-5-ene-3,4-diol	50-74	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-94
27350147-1	2016	The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity.	cholest-5-ene-3,4-diol	50-74	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	198-203
27350147-1	2016	The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity.	cholest-5-ene-3,4-diol	76-84	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-94
27350147-1	2016	The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity.	cholest-5-ene-3,4-diol	76-84	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	198-203
26805594-0	2016	Use of 4beta-hydroxycholesterol in animal and human plasma samples as a biomarker for CYP3A induction.	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	86-91
26399557-2	2016	The biomarkers 4beta-hydroxycholesterol (4betaHC) and 6beta-hydroxycortisol (6betaHCL) are sensitive to CYP3A induction and inhibition.	cholest-5-ene-3,4-diol	15-39	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	104-109
26399557-2	2016	The biomarkers 4beta-hydroxycholesterol (4betaHC) and 6beta-hydroxycortisol (6betaHCL) are sensitive to CYP3A induction and inhibition.	cholest-5-ene-3,4-diol	41-48	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	104-109
26399557-4	2016	We investigated whether endogenous plasma biomarkers (4betaHC and 6betaHCL) are associated with basal CYP3A metabolic activity in healthy subjects assessed by a convenient single-time-point oral midazolam (MDZ) phenotyping strategy.	cholest-5-ene-3,4-diol	54-61	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	102-107
27138133-0	2016	Compelling Relationship of CYP3A Induction to Levels of the Putative Biomarker 4beta-Hydroxycholesterol and Changes in Midazolam Exposure.	cholest-5-ene-3,4-diol	79-103	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	27-32
27236640-0	2016	Relationship between the plasma fentanyl and serum 4beta-hydroxycholesterol based on CYP3A5 genotype and gender in patients with cancer pain.	cholest-5-ene-3,4-diol	51-75	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	85-91
27236640-1	2016	This study aimed to evaluate the relationship between the concentrations of plasma fentanyl and serum 4beta-hydroxycholesterol based on CYP3A5 genotype and gender in cancer patients.	cholest-5-ene-3,4-diol	102-126	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	136-142
27236640-6	2016	The serum 4beta-hydroxycholesterol concentration and its ratio to total cholesterol were significantly lower in the CYP3A5*3/*3 group than in the *1 allele carrier group.	cholest-5-ene-3,4-diol	10-34	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	116-122
27236640-10	2016	In conclusion, CYP3A5*3 and gender affected the plasma fentanyl and serum 4beta-hydroxycholesterol concentrations in cancer patients.	cholest-5-ene-3,4-diol	74-98	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	15-21
26805594-1	2016	BACKGROUND: 4beta-hydroxycholesterol (4betaHC) has recently been proposed as a potential endogenous biomarker for CYP3A activity.	cholest-5-ene-3,4-diol	12-36	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	114-119
26805594-1	2016	BACKGROUND: 4beta-hydroxycholesterol (4betaHC) has recently been proposed as a potential endogenous biomarker for CYP3A activity.	cholest-5-ene-3,4-diol	38-45	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	114-119
26805594-4	2016	CONCLUSION: These assays were applied to multiple studies and demonstrated potential applications of 4betaHC as a CYP3A biomarker across preclinical and clinical settings.	cholest-5-ene-3,4-diol	101-108	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	114-119
26654672-0	2015	CYP3A activity based on plasma 4beta-hydroxycholesterol during the early postpartum period has an effect on the plasma disposition of amlodipine.	cholest-5-ene-3,4-diol	31-55	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-5
26574235-0	2016	4beta-hydroxycholesterol correlates with dose but not steady-state concentration of carbamazepine: indication of intestinal CYP3A in biomarker formation?	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	124-129
26574235-1	2016	AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine.	cholest-5-ene-3,4-diol	5-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	58-63
26574235-1	2016	AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine.	cholest-5-ene-3,4-diol	5-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	110-116
26773964-2	2015	The aim of this study was to evaluate the influence of CYP3A5 polymorphism on the increase in CYP3A activity after living kidney transplantation, by measuring the plasma concentration of 4beta-hydroxycholesterol.	cholest-5-ene-3,4-diol	187-211	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	55-61
26773964-2	2015	The aim of this study was to evaluate the influence of CYP3A5 polymorphism on the increase in CYP3A activity after living kidney transplantation, by measuring the plasma concentration of 4beta-hydroxycholesterol.	cholest-5-ene-3,4-diol	187-211	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	55-60
26654672-1	2015	This study aimed to evaluate plasma 4beta-hydroxycholesterol as an endogenous marker of CYP3A4/5 activity in early postpartum women and its impact on the plasma disposition of amlodipine.	cholest-5-ene-3,4-diol	36-60	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	88-94
26654672-10	2015	In conclusion, early postpartum women possessed higher CYP3A activity based on plasma 4beta-hydroxycholesterol and had a large pharmacokinetic variability in amlodipine.	cholest-5-ene-3,4-diol	86-110	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	55-60
27022466-7	2015	A significant association between circulatory miR-27b levels and 4beta-hydroxycholesterol ratio was found; P = 0.04, and between hepatic miR-27b levels and CYP3A activity, measured by dextromethorphan N-demethylation in human liver (P = 0.04).	cholest-5-ene-3,4-diol	65-89	microRNA 27b	Homo sapiens	46-53
26119961-0	2015	4beta-hydroxycholesterol as an endogenous CYP3A marker in cancer patients treated with taxanes.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	42-47
26231377-5	2015	CYP3A activity was determined in healthy volunteers and subjects with biopsy-proven NAFLD by oral midazolam phenotyping and measurement of plasma 4beta-hydroxycholesterol, an endogenous metabolic biomarker.	cholest-5-ene-3,4-diol	146-170	cytochrome P450, family 3, subfamily a, polypeptide 11	Mus musculus	0-5
26119961-3	2015	In this study, we evaluated the endogenous CYP3A4 marker 4beta-hydroxycholesterol (4beta-OHC) as a potential individual taxane PK predictor.	cholest-5-ene-3,4-diol	57-81	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	43-49
24964282-1	2014	A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations.	cholest-5-ene-3,4-diol	223-247	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-95
25096076-0	2014	Pharmacokinetic and pharmacogenomic modelling of the CYP3A activity marker 4beta-hydroxycholesterol during efavirenz treatment and efavirenz/rifampicin co-treatment.	cholest-5-ene-3,4-diol	75-99	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	53-58
24837659-0	2014	Validation of 4beta-hydroxycholesterol and evaluation of other endogenous biomarkers for the assessment of CYP3A activity in healthy subjects.	cholest-5-ene-3,4-diol	14-38	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	107-112
24837659-12	2014	CONCLUSIONS: Changes in plasma 4betaHC can be utilized as a surrogate for MDZ PK after multiple doses of potent CYP3A inducers.	cholest-5-ene-3,4-diol	31-38	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	112-117
24837659-13	2014	There is a more limited dynamic range for 4betaHC for assessment of potential CYP3A inhibitors.	cholest-5-ene-3,4-diol	42-49	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	78-83
24839948-11	2014	CONCLUSIONS: Both 6betaCR and 4betaHC levels showed a good dynamic response range upon strong CYP3A4 induction with rifampicin.	cholest-5-ene-3,4-diol	30-37	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	94-100
24839948-12	2014	Because of lower inter- and intrasubject variability, 4betaHC appeared more reliable and better predictive of CYP3A4 activity compared with 6betaCR.	cholest-5-ene-3,4-diol	54-61	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	110-116
24964282-0	2014	Evaluation of 4beta-Hydroxycholesterol as a Clinical Biomarker of CYP3A4 Drug Interactions Using a Bayesian Mechanism-Based Pharmacometric Model.	cholest-5-ene-3,4-diol	14-38	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	66-72
24964282-1	2014	A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations.	cholest-5-ene-3,4-diol	223-247	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	68-87
24964282-1	2014	A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations.	cholest-5-ene-3,4-diol	249-256	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	68-87
24964282-1	2014	A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations.	cholest-5-ene-3,4-diol	249-256	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-95
24964282-2	2014	Simulations from the model demonstrated that the dynamic range of 4betaHC as a biomarker of CYP3A4 induction or inhibition was narrower than that of midazolam; an inhibitor that increases midazolam area under the curve by 20-fold may only result in a 20% decrease in 4betaHC after 14 days of dosing.	cholest-5-ene-3,4-diol	66-73	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	92-98
24964282-3	2014	Likewise, an inducer that elevates CYP3A4 activity by 1.2-fold would reduce the area under the curve of midazolam by 50% but would only increase 4betaHC levels by 20% after 14 days of dosing.	cholest-5-ene-3,4-diol	145-152	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	35-41
24861746-1	2014	4beta-Hydroxycholesterol (4beta-HC) has been proposed as a new endogenous biomarker for cytochrome P450 3A4/5 activity.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	88-107
24861746-1	2014	4beta-Hydroxycholesterol (4beta-HC) has been proposed as a new endogenous biomarker for cytochrome P450 3A4/5 activity.	cholest-5-ene-3,4-diol	26-34	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	88-107
24595680-0	2014	4beta-Hydroxycholesterol as an endogenous biomarker of CYP3A activity in cynomolgus monkeys.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	55-60
24595680-1	2014	It has been proposed that in humans 4beta-hydroxycholesterol is formed mainly by CYP3A-catalyzed metabolism of cholesterol and thus may serve as an endogenous marker for CYP3A activity.	cholest-5-ene-3,4-diol	36-60	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	81-86
24595680-10	2014	The Km values of CYP3A8 and CYP3A5 for 4beta-hydroxycholesterol formation from cholesterol were 204 and 104 muM, respectively, and Vmax values were 0.600 and 0.310 pg/pmol/min, respectively.	cholest-5-ene-3,4-diol	39-63	cytochrome P450 family 3 subfamily A member 4	Macaca fascicularis	17-23
24595680-1	2014	It has been proposed that in humans 4beta-hydroxycholesterol is formed mainly by CYP3A-catalyzed metabolism of cholesterol and thus may serve as an endogenous marker for CYP3A activity.	cholest-5-ene-3,4-diol	36-60	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	170-175
24595680-3	2014	In the current study, the potential application of 4beta-hydroxycholesterol as an endogenous biomarker of CYP3A in response to drug treatment was evaluated in cynomolgus monkeys.	cholest-5-ene-3,4-diol	51-75	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	106-111
24595680-10	2014	The Km values of CYP3A8 and CYP3A5 for 4beta-hydroxycholesterol formation from cholesterol were 204 and 104 muM, respectively, and Vmax values were 0.600 and 0.310 pg/pmol/min, respectively.	cholest-5-ene-3,4-diol	39-63	cytochrome P450 family 3 subfamily A member 5	Macaca fascicularis	28-34
24595680-4	2014	Following multiple oral administration of rifampicin (a known CYP3A inducer) at 15 mg/kg/d in cynomolgus monkeys, the mean serum 4beta-hydroxycholesterol levels increased 4-fold from the baseline of 55.3 +- 21.7 to 221 +- 53.4 ng/ml.	cholest-5-ene-3,4-diol	129-153	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	62-67
24595680-11	2014	The results suggest that 4beta-hydroxycholesterol can be used as an endogenous biomarker to identify strong CYP3A inducers in cynomolgus monkeys, which may help to evaluate drug-drug interaction potential of drug candidates in preclinical settings.	cholest-5-ene-3,4-diol	25-49	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	108-113
24595680-9	2014	The formation of 4beta-hydroxycholesterol from cholesterol was specifically mediated by recombinant cynomolgus CYP3A8 and CYP3A5.	cholest-5-ene-3,4-diol	17-41	cytochrome P450 family 3 subfamily A member 4	Macaca fascicularis	111-117
24595680-9	2014	The formation of 4beta-hydroxycholesterol from cholesterol was specifically mediated by recombinant cynomolgus CYP3A8 and CYP3A5.	cholest-5-ene-3,4-diol	17-41	cytochrome P450 family 3 subfamily A member 5	Macaca fascicularis	122-128
24135442-0	2014	Association of plasma concentration of 4beta-hydroxycholesterol with CYP3A5 polymorphism and plasma concentration of indoxyl sulfate in stable kidney transplant recipients.	cholest-5-ene-3,4-diol	39-63	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	69-75
24135442-5	2014	Plasma concentrations of 4beta-hydroxycholesterol were 57.1 +- 11.2, 42.1 +- 11.8, and 34.5 +- 7.3 ng/ml in recipients with CYP3A5*1/*1 (n = 5), *1/*3 (n = 15), and *3/*3 (n = 25) genotypes, respectively, with significant differences between three genotypes.	cholest-5-ene-3,4-diol	25-49	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	124-130
24135442-7	2014	Multiple regression analysis identified the number of CYP3A5*3 alleles in genotype, plasma concentration of 3-INDS, and body weight as independent variables associated with plasma concentration of 4beta-hydroxycholesterol.	cholest-5-ene-3,4-diol	197-221	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	54-60
23089673-1	2013	We investigated the effects of pharmacogenetic variations and efavirenz pharmacokinetics on inter-individual differences in the extent of CYP3A induction by efavirenz using 4beta-hydroxycholesterol/cholesterol (4beta-OHC/Chol) as a marker for CYP3A induction.	cholest-5-ene-3,4-diol	173-197	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	138-143
23833241-3	2013	In this study, we evaluated the effect of renal function on CYP3A activity after kidney transplantation in patients with end-stage renal disease (ESRD) by measuring the change in CYP3A activity using plasma concentration of 4beta-hydroxycholesterol as a biomarker.	cholest-5-ene-3,4-diol	224-248	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	60-65
23386704-1	2013	The primary aim was to study the relationship between individual serum levels of 25-hydroxyvitamin D and 4beta-hydroxycholesterol, which is an endogenous biomarker of the drug-metabolizing CYP3A enzymes.	cholest-5-ene-3,4-diol	105-129	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	189-194
23674608-0	2013	Comparison of endogenous 4beta-hydroxycholesterol with midazolam as markers for CYP3A4 induction by rifampicin.	cholest-5-ene-3,4-diol	25-49	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	80-86
23386704-11	2013	However, the negative correlation between CRP and 4beta-hydroxycholesterol supports earlier experimental results that inflammation may suppress hepatic CYP3A activity, a finding of potentially high clinical relevance that warrants further exploration.	cholest-5-ene-3,4-diol	50-74	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	152-157
23386704-0	2013	Serum levels of 25-hydroxyvitamin D and the CYP3A biomarker 4beta-hydroxycholesterol in a high-dose vitamin D supplementation study.	cholest-5-ene-3,4-diol	60-84	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	44-49
21728364-1	2011	It has recently been proposed that plasma levels of 4beta-hydroxycholesterol (4betaHC) may be indicative of cytochrome P450 3A4 (P450 3A) activity and therefore could be used to probe for P450 3A-mediated drug-drug interactions.	cholest-5-ene-3,4-diol	52-76	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	108-127
23220593-5	2013	Only 4beta-hydroxycholesterol is a LXRalpha and beta agonist.	cholest-5-ene-3,4-diol	5-29	nuclear receptor subfamily 1, group H, member 3	Mus musculus	35-52
21728364-1	2011	It has recently been proposed that plasma levels of 4beta-hydroxycholesterol (4betaHC) may be indicative of cytochrome P450 3A4 (P450 3A) activity and therefore could be used to probe for P450 3A-mediated drug-drug interactions.	cholest-5-ene-3,4-diol	78-85	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	108-127
21507593-1	2011	A novel liquid chromatography-tandem mass spectrometry method is described for the quantitative determination of the endogenous CYP 3A4/5 marker 4beta-hydroxycholesterol in human K(2)-EDTA plasma.	cholest-5-ene-3,4-diol	145-169	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	128-135
20231858-7	2011	CYP3A5 genotype significantly correlated with the plasma 4beta-hydroxycholesterol concentration (P=0.003) and 4beta-hydroxycholesterol/cholesterol ratio (P=0.0002).	cholest-5-ene-3,4-diol	57-81	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	0-6
20231858-7	2011	CYP3A5 genotype significantly correlated with the plasma 4beta-hydroxycholesterol concentration (P=0.003) and 4beta-hydroxycholesterol/cholesterol ratio (P=0.0002).	cholest-5-ene-3,4-diol	110-134	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	0-6
20231858-10	2011	A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity.	cholest-5-ene-3,4-diol	40-64	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	114-119
20231858-8	2011	The omeprazole/omeprazole sulfone ratio was significantly correlated with 4beta-hydroxycholesterol and 4beta-hydroxycholesterol/cholesterol ratio in CYP3A5*0/*0 genotypes but not in individuals carrying the CYP3A5*1 allele.	cholest-5-ene-3,4-diol	103-127	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	149-155
20231858-10	2011	A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity.	cholest-5-ene-3,4-diol	40-64	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	130-136
18458892-0	2008	CYP3A induction and inhibition by different antiretroviral regimens reflected by changes in plasma 4beta-hydroxycholesterol levels.	cholest-5-ene-3,4-diol	99-123	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-5
20231858-10	2011	A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity.	cholest-5-ene-3,4-diol	40-64	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	142-148
20231858-10	2011	A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity.	cholest-5-ene-3,4-diol	40-64	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	214-220
21219398-0	2011	4beta-Hydroxycholesterol, an endogenous marker of CYP3A4/5 activity in humans.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	50-56
21219398-1	2011	We have proposed that 4beta-hydroxycholesterol (4beta-OHC) may be used as an endogenous marker of CYP3A activity.	cholest-5-ene-3,4-diol	22-46	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	98-103
20197489-0	2010	Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric?	cholest-5-ene-3,4-diol	34-58	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	83-101
20197489-0	2010	Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric?	cholest-5-ene-3,4-diol	34-58	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	103-108
20197489-1	2010	Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A).	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	87-105
20197489-1	2010	Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A).	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	107-112
20197489-1	2010	Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A).	cholest-5-ene-3,4-diol	33-40	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	87-105
20197489-1	2010	Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A).	cholest-5-ene-3,4-diol	33-40	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	107-112
20197489-2	2010	To assess its utility as a CYP3A metric, a pharmacokinetic model, assuming no alteration in cholesterol plasma concentrations, was developed to simulate the effect of CYP3A induction and inhibition on 4betaHC plasma levels under different treatment durations.	cholest-5-ene-3,4-diol	201-208	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	167-172
20197489-5	2010	On the other hand, simulations indicated that at least 2 weeks of dosing would be needed to detect the potent inhibition of CYP3A (maximal ~40% decrease in 4betaHC plasma levels).	cholest-5-ene-3,4-diol	156-163	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	124-129
19954708-0	2009	4beta-hydroxycholesterol as a marker of CYP3A4 inhibition in vivo - effects of itraconazole in man.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	40-46
19954708-2	2009	Here, we study the potential endogenous serum marker of CYP3A4 activity, 4beta-hydroxycholesterol, during therapy with itraconazole.	cholest-5-ene-3,4-diol	73-97	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	56-62
19954708-9	2009	Absolute and cholesterol-corrected concentrations of 4beta-hydroxycholesterol, formed by CYP3A4-mediated oxidation, decreased significantly during both cycles, on average by 29.1% (p = 0.0006) and 20.8% (p = 0.0062), respectively.	cholest-5-ene-3,4-diol	53-77	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-95
19954708-11	2009	CONCLUSIONS: In conclusion, 4beta-hydroxycholesterol appears to be a sensitive endogenous surrogate marker in human serum for inhibition of CYP3A4 by itraconazole.	cholest-5-ene-3,4-diol	28-52	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	140-146
19458613-0	2009	Plasma 4beta-hydroxycholesterol: an endogenous CYP3A metric?	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	47-52
19006545-0	2009	4beta-hydroxycholesterol as an endogenous marker for CYP3A4/5 activity.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	53-59
19006545-3	2009	We have previously shown that plasma 4beta-hydroxycholesterol continues to increase for several weeks after maximal induction of CYP3A4/5 by carbamazepine at the dose given.	cholest-5-ene-3,4-diol	37-61	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	129-135
19006545-4	2009	In the present study we aimed to determine the time course of the decrease in plasma 4beta-hydroxycholesterol after termination of induction of CYP3A4/5 by rifampicin.	cholest-5-ene-3,4-diol	85-109	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	144-150
19006545-14	2009	CONCLUSIONS: After termination of induction of CYP3A4/5, plasma 4beta-hydroxycholesterol levels decreased slowly during 8 weeks.	cholest-5-ene-3,4-diol	64-88	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	47-53
18458892-1	2008	OBJECTIVE AND METHODS: A member of the major human cytochrome P450 superfamily of hemoproteins, CYP3A4/5, converts cholesterol into 4beta-hydroxycholesterol.	cholest-5-ene-3,4-diol	132-156	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	96-102
18458892-7	2008	CONCLUSION: Changes in plasma 4beta-hydroxycholesterol following the initiation of efavirenz- or atazanavir/ritonavir-based antiretroviral therapy reflected the respective net increase and decrease of CYP3A activity of these regimens.	cholest-5-ene-3,4-diol	30-54	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	201-206
18279471-1	2008	WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: CYP3A4 converts cholesterol into 4beta-hydroxycholesterol.	cholest-5-ene-3,4-diol	75-99	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	42-48
18279471-2	2008	We have suggested that 4beta-hydroxycholesterol could be used as a clinical marker for CYP3A4 activity aiding in dose adjustments.	cholest-5-ene-3,4-diol	23-47	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	87-93
18279471-4	2008	WHAT THIS STUDY ADDS: The concentration of 4beta-hydroxycholesterol increases very slowly during CYP3A4/5 induction in paediatric patients.	cholest-5-ene-3,4-diol	43-67	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	97-103
11514559-7	2001	Recombinant CYP3A4 was shown to convert cholesterol to 4beta-hydroxycholesterol, whereas no conversion was observed with CYP1A2, CYP2C9, or CYP2B6.	cholest-5-ene-3,4-diol	55-79	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	12-18
18300941-0	2008	4Beta-hydroxycholesterol is a new endogenous CYP3A marker: relationship to CYP3A5 genotype, quinine 3-hydroxylation and sex in Koreans, Swedes and Tanzanians.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	45-50
18300941-0	2008	4Beta-hydroxycholesterol is a new endogenous CYP3A marker: relationship to CYP3A5 genotype, quinine 3-hydroxylation and sex in Koreans, Swedes and Tanzanians.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	75-81
18300941-1	2008	OBJECTIVES: To study the potential endogenous marker of CYP3A activity, 4beta-hydroxycholesterol, and its relation to sex and the CYP3A5 geno/haplotypes and compare with CYP3A4/5 catalyzed 3-hydroxylation of quinine in the three major races.	cholest-5-ene-3,4-diol	72-96	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	130-136
11514559-0	2001	Antiepileptic drugs increase plasma levels of 4beta-hydroxycholesterol in humans: evidence for involvement of cytochrome p450 3A4.	cholest-5-ene-3,4-diol	46-70	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	110-129
18300941-12	2008	Both 4beta-hydroxycholesterol and quinine/3-hydroxyquinine metabolic ratio showed a higher CYP3A activity in women than in men.	cholest-5-ene-3,4-diol	5-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	91-96
18300941-13	2008	The results give strong evidence that the plasma concentration of 4beta-hydroxycholesterol may be used as an endogenous marker of CYP3A activity (CYP3A4+5).	cholest-5-ene-3,4-diol	66-90	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	130-135
18300941-13	2008	The results give strong evidence that the plasma concentration of 4beta-hydroxycholesterol may be used as an endogenous marker of CYP3A activity (CYP3A4+5).	cholest-5-ene-3,4-diol	66-90	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	146-152
33822485-4	2021	The in vivo CYP3A4 induction effect of ivosidenib was quantified using 4beta-hydroxycholesterol and was subsequently verified with the PK data from an ivosidenib and venetoclax combination study.	cholest-5-ene-3,4-diol	71-95	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	12-18
16847425-5	2006	The plasma concentration of 4beta-hydroxycholesterol, an endogenous marker of CYP3A4 activity, was measured before and after administration of 600 mg rifampicin once daily for 9-11 days.	cholest-5-ene-3,4-diol	28-52	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	78-84
16847425-9	2006	However, the present study had sufficient power to detect only a considerably smaller rifampicin-induced increase in 4beta-hydroxycholesterol in carriers of the SLCO1B1 c.521C allele compared to subjects with the reference genotype.	cholest-5-ene-3,4-diol	117-141	solute carrier organic anion transporter family member 1B1	Homo sapiens	161-168
34703500-7	2021	However, plasma 4beta-HC was not affected by KTZ treatment despite it being a Cyp3a metabolite of cholesterol.	cholest-5-ene-3,4-diol	16-24	cytochrome P450, family 3, subfamily a, polypeptide 62	Rattus norvegicus	78-83
34580385-6	2021	We measured CYP3A4 activity using 4beta-hydroxycholesterol, an endogenous metabolite.	cholest-5-ene-3,4-diol	34-58	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	12-18
34572915-0	2021	CYP3A Activity in End-of-Life Cancer Patients Measured by 4beta-Hydroxycholesterol/cholesterol Ratio, in Men and Women.	cholest-5-ene-3,4-diol	58-82	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-5
34572915-2	2021	The aim of this study was to investigate if the CYP3A activity, measured by the endogenous marker 4beta-hydroxycholesterol/cholesterol ratio (4beta-OHC/C), is changed during the last weeks and days of life in men and women.	cholest-5-ene-3,4-diol	98-122	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	48-53
35181316-1	2022	4beta-Hydroxycholesterol (4beta-OHC) is formed by CYP3A4 and CYP3A5 and has drawn attention as an endogenous phenotyping probe for CYP3A activity.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	50-56
35229613-2	2022	We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24-hour blood pressure (BP) and plasma 4beta-hydroxycholesterol (4betaHC), agonist for liver X receptor (LXR).	cholest-5-ene-3,4-diol	154-161	nuclear receptor subfamily 1 group I member 2	Homo sapiens	40-59
35229613-2	2022	We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24-hour blood pressure (BP) and plasma 4beta-hydroxycholesterol (4betaHC), agonist for liver X receptor (LXR).	cholest-5-ene-3,4-diol	154-161	nuclear receptor subfamily 1 group I member 2	Homo sapiens	61-64
35229613-2	2022	We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24-hour blood pressure (BP) and plasma 4beta-hydroxycholesterol (4betaHC), agonist for liver X receptor (LXR).	cholest-5-ene-3,4-diol	128-152	nuclear receptor subfamily 1 group I member 2	Homo sapiens	40-59
35229613-2	2022	We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24-hour blood pressure (BP) and plasma 4beta-hydroxycholesterol (4betaHC), agonist for liver X receptor (LXR).	cholest-5-ene-3,4-diol	128-152	nuclear receptor subfamily 1 group I member 2	Homo sapiens	61-64
35181316-1	2022	4beta-Hydroxycholesterol (4beta-OHC) is formed by CYP3A4 and CYP3A5 and has drawn attention as an endogenous phenotyping probe for CYP3A activity.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	61-67
35181316-1	2022	4beta-Hydroxycholesterol (4beta-OHC) is formed by CYP3A4 and CYP3A5 and has drawn attention as an endogenous phenotyping probe for CYP3A activity.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	131-136
32896622-9	2020	The mechanism of steatosis was increased expression of Srebp1 (positive regulator of liver lipogenesis) through activation of the liver X receptor by increased oxysterols in the CA-fed rats, especially 4beta-hydroxycholesterol (4betaOH) formed by upregulated expression of hepatic Cyp3a2, responsible for 4betaOH formation.	cholest-5-ene-3,4-diol	202-226	sterol regulatory element binding transcription factor 1	Rattus norvegicus	55-61
33201347-1	2021	PURPOSE: The antifungal drugs ketoconazole and itraconazole reduce serum concentrations of 4beta-hydroxycholesterol, which is a validated marker for hepatic cytochrome P450 (CYP) 3A4 activity.	cholest-5-ene-3,4-diol	91-115	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	157-182
33631213-0	2021	4beta-hydroxycholesterol is a pro-lipogenic factor that promotes SREBP1c expression and activity through Liver X-receptor.	cholest-5-ene-3,4-diol	0-24	sterol regulatory element binding transcription factor 1	Mus musculus	65-72
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	19-43	sterol regulatory element binding transcription factor 1	Mus musculus	201-245
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	19-43	sterol regulatory element binding transcription factor 1	Mus musculus	247-254
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	19-43	sterol regulatory element binding factor 2	Mus musculus	312-318
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	45-53	sterol regulatory element binding transcription factor 1	Mus musculus	201-245
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	45-53	sterol regulatory element binding transcription factor 1	Mus musculus	247-254
33631213-3	2021	Here, we show that 4beta-hydroxycholesterol (4beta-HC), a liver and serum abundant oxysterol of poorly defined function, is a potent and selective inducer of the master lipogenic transcription factor, Sterol Regulatory Element Binding Protein 1c (SREBP1c), but not the related steroidogenic transcription factor SREBP2.	cholest-5-ene-3,4-diol	45-53	sterol regulatory element binding factor 2	Mus musculus	312-318
33631213-4	2021	By correlating tracing of lipid synthesis with lipogenic gene expression profiling, we found that 4beta-HC acts as a putative agonist for Liver X receptor (LXR), a sterol sensor and transcriptional regulator previously linked to SREBP1c activation.	cholest-5-ene-3,4-diol	98-106	nuclear receptor subfamily 1, group H, member 3	Mus musculus	138-154
33631213-4	2021	By correlating tracing of lipid synthesis with lipogenic gene expression profiling, we found that 4beta-HC acts as a putative agonist for Liver X receptor (LXR), a sterol sensor and transcriptional regulator previously linked to SREBP1c activation.	cholest-5-ene-3,4-diol	98-106	nuclear receptor subfamily 1, group H, member 3	Mus musculus	156-159
33631213-4	2021	By correlating tracing of lipid synthesis with lipogenic gene expression profiling, we found that 4beta-HC acts as a putative agonist for Liver X receptor (LXR), a sterol sensor and transcriptional regulator previously linked to SREBP1c activation.	cholest-5-ene-3,4-diol	98-106	sterol regulatory element binding transcription factor 1	Mus musculus	229-236
33631213-7	2021	Thus, 4beta-HC is an endogenous regulator of de novo lipogenesis through the LXR-SREBP1c axis.	cholest-5-ene-3,4-diol	6-14	nuclear receptor subfamily 1, group H, member 3	Mus musculus	77-80
33631213-7	2021	Thus, 4beta-HC is an endogenous regulator of de novo lipogenesis through the LXR-SREBP1c axis.	cholest-5-ene-3,4-diol	6-14	sterol regulatory element binding transcription factor 1	Mus musculus	81-88
32896622-9	2020	The mechanism of steatosis was increased expression of Srebp1 (positive regulator of liver lipogenesis) through activation of the liver X receptor by increased oxysterols in the CA-fed rats, especially 4beta-hydroxycholesterol (4betaOH) formed by upregulated expression of hepatic Cyp3a2, responsible for 4betaOH formation.	cholest-5-ene-3,4-diol	228-235	sterol regulatory element binding transcription factor 1	Rattus norvegicus	55-61
32896622-9	2020	The mechanism of steatosis was increased expression of Srebp1 (positive regulator of liver lipogenesis) through activation of the liver X receptor by increased oxysterols in the CA-fed rats, especially 4beta-hydroxycholesterol (4betaOH) formed by upregulated expression of hepatic Cyp3a2, responsible for 4betaOH formation.	cholest-5-ene-3,4-diol	305-312	sterol regulatory element binding transcription factor 1	Rattus norvegicus	55-61
32344455-7	2020	The 4betaHC, an agonist for liver X receptor (LXR), induced renin expression modestly in LXR-alpha expressing Calu-6 cells but only at unphysiologically high 4betaHC concentrations.	cholest-5-ene-3,4-diol	4-11	renin	Homo sapiens	60-65
33182477-7	2020	In addition, plasma 4beta-hydroxycholesterol (4betaHC), formed under the control of PXR in the liver, is associated with lower blood pressure in healthy volunteers.	cholest-5-ene-3,4-diol	20-44	nuclear receptor subfamily 1 group I member 2	Homo sapiens	84-87
33182477-7	2020	In addition, plasma 4beta-hydroxycholesterol (4betaHC), formed under the control of PXR in the liver, is associated with lower blood pressure in healthy volunteers.	cholest-5-ene-3,4-diol	46-53	nuclear receptor subfamily 1 group I member 2	Homo sapiens	84-87
32344455-7	2020	The 4betaHC, an agonist for liver X receptor (LXR), induced renin expression modestly in LXR-alpha expressing Calu-6 cells but only at unphysiologically high 4betaHC concentrations.	cholest-5-ene-3,4-diol	4-11	nuclear receptor subfamily 1 group H member 3	Homo sapiens	89-98
32656158-4	2020	To specifically and quickly measure CYP3A activity, we developed method based on gas chromatography interfaced with triple-quadrupole mass spectrometry for the quantification of cortisol, cortisone, 6beta-hydroxycortisol, and 6beta-hydroxycortisone simultaneously in urine and 4beta-hydroxycholesterol in plasma.	cholest-5-ene-3,4-diol	277-301	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	36-41
32537715-7	2020	The mean plasma Day 14/Day 1 ratio of 4beta-hydroxycholesterol, an endogenous biomarker of CYP3A4 activity, was 0.59 (90% CI 0.54-0.66), suggesting a net inhibition of CYP3A4 by fedratinib.	cholest-5-ene-3,4-diol	38-62	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	91-97
32537715-7	2020	The mean plasma Day 14/Day 1 ratio of 4beta-hydroxycholesterol, an endogenous biomarker of CYP3A4 activity, was 0.59 (90% CI 0.54-0.66), suggesting a net inhibition of CYP3A4 by fedratinib.	cholest-5-ene-3,4-diol	38-62	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	168-174
32292343-1	2020	Activation of pregnane X receptor (PXR) elevates circulating 4beta-hydroxycholesterol (4betaHC), an agonist of liver X receptor (LXR).	cholest-5-ene-3,4-diol	61-85	nuclear receptor subfamily 1 group I member 2	Homo sapiens	14-33
32292343-1	2020	Activation of pregnane X receptor (PXR) elevates circulating 4beta-hydroxycholesterol (4betaHC), an agonist of liver X receptor (LXR).	cholest-5-ene-3,4-diol	61-85	nuclear receptor subfamily 1 group I member 2	Homo sapiens	35-38
32292343-1	2020	Activation of pregnane X receptor (PXR) elevates circulating 4beta-hydroxycholesterol (4betaHC), an agonist of liver X receptor (LXR).	cholest-5-ene-3,4-diol	87-94	nuclear receptor subfamily 1 group I member 2	Homo sapiens	14-33
32292343-1	2020	Activation of pregnane X receptor (PXR) elevates circulating 4beta-hydroxycholesterol (4betaHC), an agonist of liver X receptor (LXR).	cholest-5-ene-3,4-diol	87-94	nuclear receptor subfamily 1 group I member 2	Homo sapiens	35-38
31002385-0	2019	Use of 4beta-Hydroxycholesterol Plasma Concentrations as an Endogenous Biomarker of CYP3A Activity: Clinical Validation in Individuals With Type 2 Diabetes.	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	84-89
30058048-3	2019	We describe the utility of 4beta hydroxycholesterol as a marker of CYP3A activity.	cholest-5-ene-3,4-diol	27-51	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	67-72
30826567-0	2019	Factors involved in phenoconversion of CYP3A using 4beta-hydroxycholesterol in stable kidney transplant recipients.	cholest-5-ene-3,4-diol	51-75	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	39-44
30748026-0	2019	4beta-Hydroxycholesterol as an Endogenous Biomarker for CYP3A Activity: Literature Review and Critical Evaluation.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	56-61
30748026-2	2019	Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal.	cholest-5-ene-3,4-diol	17-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	73-78
30748026-2	2019	Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal.	cholest-5-ene-3,4-diol	17-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	163-168
30748026-2	2019	Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal.	cholest-5-ene-3,4-diol	17-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	163-168
30826567-4	2019	We measured plasma concentrations of the above compounds in stable kidney transplant recipients, and evaluated their relations with phenoconversion of CYP3A evaluated by plasma concentration of 4beta-hydroxycholesterol, a biomarker of CYP3A activity.	cholest-5-ene-3,4-diol	194-218	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	151-156
30826567-8	2019	RESULTS: Significantly higher plasma 4beta-hydroxycholesterol concentration was observed in recipients with CYP3A5*1 allele (n = 23) compared to those without the allele (n = 40), and the cut-off value was 40.0 ng/mL.	cholest-5-ene-3,4-diol	37-61	cytochrome P450 family 3 subfamily A member 5	Homo sapiens	108-114
30858735-0	2019	Modeling and simulation of the endogenous CYP3A induction marker 4beta-hydroxycholesterol during enasidenib treatment.	cholest-5-ene-3,4-diol	65-89	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	42-47
30340067-0	2018	Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance.	cholest-5-ene-3,4-diol	138-162	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	226-231
30340067-0	2018	Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance.	cholest-5-ene-3,4-diol	138-162	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	255-261
30340067-0	2018	Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance.	cholest-5-ene-3,4-diol	138-162	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	255-260
29649093-0	2018	Comparison of CYP3A4-Inducing Capacity of Enzyme-Inducing Antiepileptic Drugs Using 4beta-Hydroxycholesterol as Biomarker.	cholest-5-ene-3,4-diol	84-108	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	14-20
29991576-4	2018	CYP3A4 phenotype was measured as serum concentration of 4beta-hydroxycholesterol (4betaOHC) by ultra-performance liquid chromatography-tandem mass spectrometry in samples collected prior to and 3 months after initiation of treatment with TNF-alpha inhibitors.	cholest-5-ene-3,4-diol	56-80	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-6
29649093-3	2018	METHODS: Residual serum samples from patients treated with EIAEDs or levetiracetam were collected from a therapeutic drug monitoring service for analysis of 4beta-hydroxycholesterol (4betaOHC), which is an indicator of CYP3A4 activity.	cholest-5-ene-3,4-diol	157-181	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	219-225
29749106-1	2018	reply to "Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity?"	cholest-5-ene-3,4-diol	14-38	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	75-81
29464732-0	2018	Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity?	cholest-5-ene-3,4-diol	4-28	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	65-71
29759884-0	2018	Assessment of induced CYP3A activity in pregnant women using 4beta-hydroxycholesterol: Cholesterol ratio as an appropriate metabolic marker.	cholest-5-ene-3,4-diol	61-85	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	22-27
29691891-0	2018	Kuypers and Vanhove reply to "Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity?"	cholest-5-ene-3,4-diol	34-58	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	95-101
29759884-5	2018	RESULTS: An increased 4beta-hydroxycholesterol/cholesterol ratio, consistent with high CYP3A activity, was observed in pregnant women compared with that in non-pregnant women; however, no differences were observed among trimesters.	cholest-5-ene-3,4-diol	22-46	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	87-92
29759884-7	2018	CONCLUSIONS: We observed an increase in the activity of CYP3A following but not during pregnancy when measured using the 4beta-hydroxycholesterol/cholesterol ratio.	cholest-5-ene-3,4-diol	121-145	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	56-61
29858698-0	2018	Evaluation of 4beta-Hydroxycholesterol and 25-Hydroxycholesterol as Endogenous Biomarkers of CYP3A4: Study with CYP3A-Humanized Mice.	cholest-5-ene-3,4-diol	14-38	cytochrome P450, family 3, subfamily a, polypeptide 11	Mus musculus	93-98
29279486-2	2018	Methods The level of serum 4beta-hydroxycholesterol (4betaHC), a surrogate marker of CYP3A4 activity, was determined by LC-MS/MS in samples obtained from patients with HCV infection (CHCs) as well as healthy control subjects (CTLs).	cholest-5-ene-3,4-diol	27-51	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	85-91
29279486-2	2018	Methods The level of serum 4beta-hydroxycholesterol (4betaHC), a surrogate marker of CYP3A4 activity, was determined by LC-MS/MS in samples obtained from patients with HCV infection (CHCs) as well as healthy control subjects (CTLs).	cholest-5-ene-3,4-diol	53-60	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	85-91
29279486-10	2018	Conclusion The evaluation of CYP3A4 activity by measuring 4betaHC before treatment may provide additional information that can potentially be used to select cost- and efficacy-optimized treatment of HCV.	cholest-5-ene-3,4-diol	58-65	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	29-35
29858698-2	2018	Since the endogenous compounds 4beta-hydroxycholesterol (4beta-HC) and 25-hydroxycholesterol (25-HC) are generated from cholesterol via CYP3A enzymes, we examined whether the plasma levels of 4beta-HC and 25-HC reflect hepatic CYP3A4 activity by using a CYP3A-humanized mouse model, in which the function of endogenous Cyp3a was genetically replaced by human CYP3A.	cholest-5-ene-3,4-diol	31-55	cytochrome P450, family 3, subfamily a, polypeptide 11	Mus musculus	136-141
29858698-2	2018	Since the endogenous compounds 4beta-hydroxycholesterol (4beta-HC) and 25-hydroxycholesterol (25-HC) are generated from cholesterol via CYP3A enzymes, we examined whether the plasma levels of 4beta-HC and 25-HC reflect hepatic CYP3A4 activity by using a CYP3A-humanized mouse model, in which the function of endogenous Cyp3a was genetically replaced by human CYP3A.	cholest-5-ene-3,4-diol	57-65	cytochrome P450, family 3, subfamily a, polypeptide 11	Mus musculus	136-141
29858698-6	2018	In addition, in vitro studies using human liver microsomes showed that the formation of 4beta-HC was strongly inhibited by a CYP3A inhibitor, while the inhibitory effect of the CYP3A inhibition on the formation of 25-HC was weak.	cholest-5-ene-3,4-diol	88-96	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	125-130
28585378-0	2017	4beta-Hydroxycholesterol level significantly correlates with steady-state serum concentration of the CYP3A4 substrate quetiapine in psychiatric patients.	cholest-5-ene-3,4-diol	0-24	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	101-107
29117990-7	2018	The simulated midazolam area under the curve ratio of 0.54 and an accompanying observed 1.9-fold increase in the CYP3A4 activity of biomarker 4beta-hydroxycholesterol indicated a weak-to-moderate CYP3A4 induction by midostaurin and its metabolites at steady state in patients with advSM.	cholest-5-ene-3,4-diol	142-166	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	113-119
29117990-7	2018	The simulated midazolam area under the curve ratio of 0.54 and an accompanying observed 1.9-fold increase in the CYP3A4 activity of biomarker 4beta-hydroxycholesterol indicated a weak-to-moderate CYP3A4 induction by midostaurin and its metabolites at steady state in patients with advSM.	cholest-5-ene-3,4-diol	142-166	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	196-202
28928137-2	2017	Therefore, the aim of this study was to evaluate the change in CYP3A activity measured as 4beta-hydroxycholesterol (4betaOHC) concentration after kidney transplantation.	cholest-5-ene-3,4-diol	90-114	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	63-68
28585378-1	2017	AIM: 4beta-Hydroxycholesterol (4betaOHC) is sensitive towards induction or inhibition of CYP3A4, but its potential usefulness as a dosing biomarker remains to be demonstrated.	cholest-5-ene-3,4-diol	5-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	89-95
28603840-1	2017	AIMS: The CYP3A metric 4beta-hydroxycholesterol (4betaOHC) has been shown to correlate with tacrolimus steady-state apparent oral clearance (CL/F).	cholest-5-ene-3,4-diol	23-47	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	10-15
28146606-3	2017	The aim of this study was to assess the value of the endogenous CYP3A marker 4beta-hydroxycholesterol (4betaOHC) for tacrolimus dose individualization early after kidney transplantation.	cholest-5-ene-3,4-diol	77-101	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	64-69
27975131-1	2017	PURPOSE: Individual variability in the endogenous CYP3A metabolite 4beta-hydroxycholesterol (4betaOHC) is substantial, but to which extent this is determined by genetic and nongenetic factors remains unclear.	cholest-5-ene-3,4-diol	67-91	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	50-55
27718639-0	2017	Perspective: 4beta-hydroxycholesterol as an emerging endogenous biomarker of hepatic CYP3A.	cholest-5-ene-3,4-diol	13-37	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	85-90
27718639-3	2017	Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes.	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	97-115
27718639-3	2017	Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes.	cholest-5-ene-3,4-diol	7-31	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	117-122
27718639-3	2017	Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes.	cholest-5-ene-3,4-diol	33-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	97-115
27718639-3	2017	Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes.	cholest-5-ene-3,4-diol	33-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	117-122
27718639-5	2017	Herein, we review the biology of 4beta-HC, its response to treatment with CYP3A inducers, inhibitors and mixed inducer/inhibitors in healthy volunteers and patients, the association of 4beta-HC with other probes of CYP3A activity (e.g. midazolam, urinary cortisol ratios), and present predictive pharmacokinetic models.	cholest-5-ene-3,4-diol	33-41	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	74-79